Assay Detail
Functional
CHEMBL2182583
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonistic activity at CRTH2 in human eosinophils assessed as inhibition of PGD2-induced calcium mobilization after 60 mins by Fluo-3 based fluorescence assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Update on the development of antagonists of chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2). From lead optimization to clinical proof-of-concept in asthma and allergic rhinitis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 7.75 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2181805 | — | — | 1 | 8.22 |
| CHEMBL2181806 | — | — | 1 | 8.05 |
| CHEMBL560993 | TIMAPIPRANT | 3.0 | 1 | 7.89 |
| CHEMBL2181807 | — | — | 1 | 7.82 |
| CHEMBL2181808 | — | — | 1 | 7.36 |
| CHEMBL196707 | — | — | 1 | 7.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2181805 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL2181806 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL560993 | TIMAPIPRANT | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL2181807 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL2181808 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL196707 | — | Ki | = | 68.0 | nM | 7.17 |